Oral Peptide Dosage Form with Thermoresponsive Eutectic Core
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
The oral delivery of proteins and peptides is hindered by enzymatic degradation, low membrane permeability, and limited absorption in the gastrointestinal tract, leading to low bioavailability and challenges in patient compliance due to side effects from parenteral administration.
Innovation Solution
A thermoresponsive eutectic composition combined with a crosslinking agent and a porous polymeric composition is used to form an API-loaded region, which is protected and released in a controlled manner at the intestine, utilizing a coating to enhance absorption and protect against degradation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If proteins and peptides are administered orally, then patient compliance and ease of administration are improved, but enzymatic degradation in the gastrointestinal tract causes loss of substance and reduced bioavailability
Solution Approach 1:
The patent applies preliminary anti-action by incorporating protease inhibitors and protective coatings on the oral dosage form before administration. These protective measures prevent enzymatic degradation from occurring by counteracting the harmful proteolytic enzymes in the gastrointestinal tract, thereby preserving the integrity of the peptide or protein during its passage through the digestive system
Solution Approach 2:
The patent uses permeation enhancers and protective carriers as intermediaries between the peptide/protein and the gastrointestinal environment. These intermediaries facilitate the transport of the fragile biologic through the harsh gastrointestinal conditions, enabling it to reach the absorption site intact while protecting it from enzymatic degradation
2Reliability
If proteins and peptides are administered parenterally, then bioavailability is improved, but patient compliance deteriorates due to pain, allergic reactions, and multiple injections required
Solution Approach 1:
The patent replaces the mechanical injection system with an oral pharmaceutical dosage form. Instead of using needles and syringes to deliver the peptide or protein directly into the bloodstream, the invention uses an orally administrable tablet or capsule that releases the biologic in the gastrointestinal tract, thereby eliminating the mechanical trauma and discomfort associated with parenteral administration
3Ease of operation
If proteins and peptides are administered orally, then patient compliance is improved, but membrane permeability and absorption into systemic circulation are limited
Solution Approach 1:
The patent applies parameter changes by using permeation enhancers that temporarily modify the physical and chemical properties of the intestinal membrane. These enhancers alter the membrane's permeability parameters, allowing peptides and proteins to pass through the intestinal wall into the systemic circulation while maintaining the integrity of the oral administration route
Solution Approach 2:
The patent employs composite delivery systems that combine multiple functional components including protective coatings, permeation enhancers, and targeted release mechanisms. These composite materials work synergistically to protect the peptide or protein from degradation, enhance membrane permeability, and facilitate absorption into the systemic circulation while maintaining oral administration advantages
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
This approach allows for effective site-specific delivery of proteins and peptides to the intestine, reducing degradation and enhancing absorption, thereby improving bioavailability and patient compliance.
Implementation Method 1
a thermoresponsive eutectic composition which is solid at or about room temperature and fluid at or about body temperature
Implementation Method 2
the porous polymeric composition allowing the ingress of water to contact the crosslinking agent thereby facilitating the crosslinking agent to cause crosslinking of the porous polymeric composition
Implementation Method 3
facilitating the crosslinking agent to cause crosslinking of the porous polymeric composition
Implementation Method 4
which crosslinked porous polymeric composition allows controlled egress of API via egress of fluid thermoresponsive eutectic composition at the intestine
Data Source
AI summary
The invention relates to an oral polymeric pharmaceutical dosage form which comprises a thermoresponsive eutectic composition which is solid at or about room temperature and fluid at or about body temperature, the eutectic composition mixed together with a crosslinking agent and an active pharmaceutical ingredient (API) to form an API loaded region; and a porous polymeric composition at least partially surrounding the API loaded region to protect the API when the dosage form is in a stomach of the human or animal body, the porous polymeric composition allowing the ingress of water to contact the crosslinking agent thereby facilitating the crosslinking agent to cause crosslinking of the porous polymeric composition, which crosslinked porous polymeric composition allows controlled egress of API via egress of fluid thermoresponsive eutectic composition at the intestine. In a preferred embodiment, the dosage form further comprises a coating there around.